Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors

  • J Am Chem Soc. 2002 Oct 9;124(40):11852-3. doi: 10.1021/ja0277226.
Natalie A Dales  1 ,  Alexandra E Gould ,  James A Brown ,  Emily F Calderwood ,  Bing Guan ,  Charles A Minor ,  James M Gavin ,  Paul Hales ,  Virendar K Kaushik ,  Michael Stewart ,  Peter J Tummino ,  Chad S Vickers ,  Timothy D Ocain ,  Michael A Patane
Affiliations
  • 1. Millennium Pharmaceuticals, Inc., 75 Sidney Street, Cambridge, MA 02139, USA.
PMID: 12358520 DOI: 10.1021/ja0277226
Abstract

Angiotensin-converting enzyme-related Carboxypeptidase (ACE2) is a recently identified zinc metalloprotease with Carboxypeptidase activity that was identified using our genomics platform. We implemented a rational design approach to identify potent and selective ACE2 inhibitors. To this end, picomolar inhibitors of ACE2 were designed and synthesized.

Products